Tablets Part 2 Flashcards
what is another name for molded tablets
tablet triturates
how are tablet triturates prepared? what is another name for them?
another name = molded tablets
prepared by molding rather than compression – minimum compression force
molded tablets are usually ___ that contain ____
small, cylindrical tablets that usually contain potent drugs
molded tablets/tablet triturates are designed to be….
readily and completely soluble in water
what kind of excipients are AVOIDED in the preparation of molded tablets/tablet triturates?
any water insoluble excipient
________ tablets are designed to disintegrate and release their medication with no special rate controlling features such as special coatings and other techniques
immediate release
rapdily disintegration or dissolving tablets disintegrate or dissolve in the mouth when?
within 1 minute, and some are within 10 seconds
what are the excipients used in rapidly disintegrating or dissolving tablets and why?
very water soluble excipients because they wick (absorb) water into the tablet for rapid disintegration or dissolution
name 2 techniques used to prepare rapidly disintegrating or dissolving tablets
lypophilization or soft direct compression
name 2 products that use the lyophilization method of preparing rapidly disintegrating or dissolving tablets
zydis and claritin
name 2 tablets that use the soft direct compression method of preparing rapidly disintegrating or dissolving tablets
Dimetapp ND
Tempra Quicklets
which technique of preparing rapdily disintegrating or dissolving tablets is “freeze drying” to increase porosity and allow for it to quickly dissolve
lyophilization
true or false
the saliva from rapidly disintegrating or dissolving tablets can be swallowed
TRUE – it can. the dose is designed to go through the stomach
however, buccal and sublingual saliva should NOT be swallowed
true or false
compressed tablets must be elegant in appearance
TRUE
if not, we have to apply sugar or film coating
compressed tablets must be bioavailable.
this involves the tablet doing what?
undergoing disintegration and dissolution
compressed tablets must have uniformity in what 3 things?
weight
thickness
drug contents
true or false
it is not necessary for compressed tablets to be sufficiently strong to withstand pressures
false - it is
due to manufacturing, packaging, and shipping etc
compressed tablets must retain all functional attributes throughout…..
this involves the drug’s ___ and ___
its shelf life
stability and efficacy
the diameter and shape of compressed tablets depends on what?
the die and the punches used in compression
the MORE CONCAVE the punches, the ____ convex the compressed tablet
more convex
name 6 quality standards and compendial requirements for tablets
which of these are required for capsuels?
tablet weight and USP weight variation test
content uniformity
tablet thickness
tablet hardness and friability
tablet disintegration
tablet dissolution
only USP weight variation test and content uniformity is required for capsules
true or false
the USP weight variation test is related to the amount of API contained in the tablet
FALSE – related to the total weight of the tablet
the content uniformity test is related to the amount of API
explain how to perform tablet weight variation
if tablets are coated, weight 20 tablets individually (if uncoated, weight 10 tablets individuallt)
determine the average weight of the tablets
each INDIVIDUAL tablet should be within 10% of labeled claim. if greater than 10%, must be rejected
tablet weight variation:
for the determination of dosage form uniformity by weight variation, select not _______ tablets
not less than 30 tablets
true or false
in tablet weight variation, 10 tablets should be weighted individually if they are coated
false – 10 if uncoated
20 if coated
in the content uniformity test, how many tablets are sampled and how many are assayed?
30 tablets are sampled and 10 are assayed
in the 10 tablets assayed in the content uniformity test, explain the requirements in order to be accepted
the average content of each tablet should be within 85%-115% of the average potency (plus minus 15%)
NONE should be outside of 75%-125%
if any show potency OUTSIDE OF 85%-115%, assay 20 more tablets
to pass this:
-net content of all tablets within 75%-125%
-and the net content of only 1 tablet can be outside 85-115%
if there are more than 2 outside of the 15% range, reject whole batch
explain the tablet thickness test and requirements
the thickness and diameter of 20 tablets is measured
for thickness, variation can’t be more than 10%
for diameter, variation can’t be more than 2%
true or false
the tablet thickness test measures both thickness and diameter
true
in the tablet thickness requirements, the diameter must be within 10% and the thickness must be within 2%.
20 tablets are measured
TRUE OR FALSE
false
20 tablets are measures
average variability:
diameter must be within 2%
thickness must be within 10%
in measuring tablet hardness, what is the normal minimum quantity of force to be applied?
what is this test called?
about 4kg force applied and tablet does not break
stress test
name the 2 tests for tablet hardness
stress test - force of 4kg is applied and tablet should not break
friability (easily crumbled or broken) test - measures the tablet’s durability. weight loss must be less than 1%. 20 rotations per minute (rpm) is applied
true or false
the stress test in which 4kg is applied dto the tablet’s is a measure of the tablet’s friability
FALSE - measure of the tablet’s hardness
friability test is when it undergoes 20rpm and less than 1% of the weight can be lost to be accepted
why must a tablet be able to disintegrate?
for the medicinal agent in the tablet to be fully available for absorption, it must fully disintegrate and release the drug to the body fluids to then undergo DISSOLUTION
if the site of action is the GI tract, the tablet must disintegrate in order to increase the surface area for activity within the GI tract
the tablet disintegration test determines what?
the disintegration time of 12 tablets
6 used for every test – so 2 tests are done for a total of 12 tabs
in the tablet disintegration test, state the amount of time allowed for the full disintegration of these tablets:
uncoated
coated
buccal
sublingal
enteric coated
uncoated: no more than 15-30 minutes (30 minutes = compressed tabs)
coated - up to 2 hours
buccal - all tablets within 4 hours
sublingual - 30 seconds - 3 minutes MAX (1 min is goal)
enteric coated - stimulates gastric fluid (WATER NOT USED) for 1 hour – NO cracking or disintegration or anything can be observed after this 1 hour
time used for disintegration test for buccal tablets
all tablets must disintegrate within 4 hours
time required for disintegration test for most uncoated tablets.
what is time for compressed tablets?
most uncoated tablets = 15-30 minutes
for compressed - more like 30 mins
time required for disintegration test for coated tablets
up to 2 hours
what is the mesh used in the tablet disintegration test?
how many cycles per minute?
which fluid is used?
10 mesh
30 cycles/min
water is used for all tablets EXCEPT enteric coated
for enteric coated, a fluid with a pH of 1 is used to represent the stomach. NO disintegration of cracking or softening can be seen after the 1 hours (bc the whole point of enteric coating is for it not to be absorbed in the stomach, but in the small intestine)
what is the rate limiting step for WATER SOLUBLE tablets to provide therapeutic effect?
tablet disintegration
dissolution is not a problem for a water soluble drug
an indicator of the bioavailability of the drug from the solid dosage form is……
tablet dissolution
what is tablet dissolution?
an indicator of the bioavailability of the drug from the solid dosage form
true or false
for a water insoluble drug, disintegration is the rate determining step
FALSE - DISSOLUTION
what is the criteria for a drug to be water soluble
solubility is greater than 10mg/mL at room temp
what is the criteria for a drug to be water insoluble
solubility is less than 1mg/mL
water soluble drug: solubility greater than 10mg/mL
water insoluble drug: solubility less than 1mg/mL
what about drugs whos solubility is between 1mg/mL - 10mg/mL?? what is the rate limiting step?
both disintegration AND dissolution are important for these drugs
is there an issue?
solubility of drug: 20mg/mL
dose: 50mg
yes
there is a solubility issue.
what does IVIVC stand for
what is it related to?
in vivo in vitro correlation
related to tablet dissolution tests
what is the approximate amount of fluids that should be taken with a drug
250mL
name 3 methods of the manufacture of compressed tablets
wet granulation method
dry granulation method
direct compression tableting
name 3 common steps for the manufacture of compressed tablets
grinding the drug or powder
blending the powders
adding the lubricant
what is granulation?
process in which a powder mixture is converted to free flowing particles
name 3 benefits of performing granulation
you can get:
-desired size/distribution
-desired granule shape
-desired granule hardness and density
what is one of the most demanding processes in tablet preparation?
granulation
what is another word for dry granulation?
slugging
which method of manufacturing compressed tablets is generally used first?
wet granulation
true or false
there is NO granulation involved in the direct compression method of manufacturing compressed tablets
true
in dry granulation, a tablet mixture is prepared without….
a wet binder or moisture
(liquid)
in which method of preparing compressed tablets is a slug formed and then compressed?
in dry granulation/slugging
why is DIRECT COMPRESSION becoming a more desired method of manufacturing compressed tablets?
because of the availability of the excipients needed in this method
what is the most widely used and most general method of tablet preparation?
wet granulation
what is the most expensive method of preparing compressed tablets?
wet granulation
name 2 advantages of the wet granulation method
most reliable method
has the highest probability of meeting the requirements to make a successful tablet
name 4 disadvantages of wet granulation
-labor intensive
-time consuming
-CANNOT be used for water sensitive drugs
-a uniform granulation needs to be prepared
for wet granulation, the drug cannot be….
MOISTURE SENSITIVE
“the granulation will meet all the physical requirements for the compression of good tablets”
wet granulation
in wet granulation, how many times is the preparation screened?
explain
screened twice
1st time - after damp mass is prepared. no 6 or 8 mesh screen
after drying – screened again
12-20 mesh size (SMALLER)
Name 4 uses of lubricant in tablet preparation
improves flow from the hopper to the die
prevents adhesion to punches and dies during compression
gives sheen to the finished tablet
reduces friction between tablet and die wall during ejection
in wet granulation, how is the granulation dried?
by thermostatically controlled ovens that constantly record the time temp and humidty
